公开(公告)号：US07910612B2

公开(公告)日：2011-03-22

申请号：US12062769

申请日：2008-04-04

Applicant: Stefanie Keil ,  Karl Schoenafinger ,  Hans Matter ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

Inventor： Stefanie Keil ,  Karl Schoenafinger ,  Hans Matter ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

IPC: A61K31/433 ,  C07D285/12

CPC classification number: C07D285/135 ,  C07D417/12

Abstract: The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract translation: 本发明包括4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其衍生物及其盐，以及其制备方法及其用作药物组合物的方法。 更具体地，本发明涉及4-氧-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARα， PPARδ和PPARgamma激动剂活性。 化合物本身由式I的结构定义，其中各种未命名的取代基在本文中定义。 该化合物适用于治疗脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其它神经变性疾病。

公开(公告)号：US07910606B2

公开(公告)日：2011-03-22

申请号：US12562276

申请日：2009-09-18

Applicant: Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Hans Matter

Inventor： Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Hans Matter

IPC: A61K31/454 ,  A61K31/415 ,  A61K31/4245 ,  C07D413/02 ,  C07D419/02 ,  C07D401/04

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.

Abstract translation: 本发明涉及式I化合物，其中R 0; R1; R2; R3; R4; Q; V，G和M具有以下含义。 式I化合物是药理活性化合物。 它表现出强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于 治疗或预防因素Xa和/或因子VIIa的抑制。 本发明还涉及制备式I化合物的方法和包含其的药物制剂。

公开(公告)号：US20110039830A1

公开(公告)日：2011-02-17

申请号：US12845317

申请日：2010-07-28

Applicant: Henning STEINHAGEN ,  Bodo SCHEIPER ,  Hans MATTER ,  Hans Ulrich STILZ ,  Gary MCCORT

Inventor： Henning STEINHAGEN ,  Bodo SCHEIPER ,  Hans MATTER ,  Hans Ulrich STILZ ,  Gary MCCORT

IPC: A61K31/551 ,  C07D403/06 ,  A61K31/454 ,  C07D401/14 ,  A61K31/4545 ,  A61P9/00 ,  A61P13/12 ,  A61P27/06

CPC classification number: C07D209/42 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04

Abstract: The present invention relates to cyclic indole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式I的环吲哚-3-甲酰胺，其中A，R，R10，R20，R30，R40，n，p和q具有权利要求中所示的含义，它们是有价值的药物活性化合物。 具体地说，它们抑制酶肾素并调节肾素 - 血管紧张素系统的活性，并且可用于治疗例如高血压等疾病。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

公开(公告)号：US07858619B2

公开(公告)日：2010-12-28

申请号：US11862818

申请日：2007-09-27

Applicant: Armin Hofmeister ,  Manfred Schudok ,  Hans Matter ,  Kristin Breitschopf ,  Antonio Ugolini

Inventor： Armin Hofmeister ,  Manfred Schudok ,  Hans Matter ,  Kristin Breitschopf ,  Antonio Ugolini

IPC: C07D401/02 ,  A61K31/47

CPC classification number: C07D217/26 ,  C07D403/12

Abstract: The present invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.

Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，A，L和n如本文所定义，其药物组合物，制剂和用作MMP抑制剂。

公开(公告)号：US20100240580A1

公开(公告)日：2010-09-23

申请号：US12708179

申请日：2010-02-18

Applicant: Gerhard ZOLLER ,  Marc Dietrich VOSS ,  Hans MATTER ,  Andreas HERLING ,  Christophe Philippo ,  Claudie NAMANE ,  Juan-Antonio SANCHEZ-ARIAS

Inventor： Gerhard ZOLLER ,  Marc Dietrich VOSS ,  Hans MATTER ,  Andreas HERLING ,  Christophe Philippo ,  Claudie NAMANE ,  Juan-Antonio SANCHEZ-ARIAS

IPC: A61K38/28 ,  C07D235/18 ,  A61K31/4184 ,  A61P3/10 ,  A61P3/04 ,  A61P5/50 ,  A61P25/28 ,  A61P9/00 ,  A61P3/06 ,  A61P25/18 ,  C07D401/12 ,  A61K31/4439 ,  C07D409/12 ,  C07D417/12 ,  A61K31/427 ,  A61K38/27 ,  A61K31/48 ,  A61P5/06

CPC classification number: C07D235/18 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12

Abstract: The invention relates to azoloarine derivatives of formula I wherein R, A, B, D, Y, X, M and W are as defined herein, and their physiologically tolerated salts.

Abstract translation: 本发明涉及式I的偶氮合成衍生物，其中R，A，B，D，Y，X，M和W如本文所定义，以及它们的生理上耐受的盐。

公开(公告)号：US20090130209A1

公开(公告)日：2009-05-21

申请号：US12359754

申请日：2009-01-26

Applicant: Swen HOELDER ,  Gunter MULLER ,  Karl SCHOENAFINGER ,  David William WILL ,  Hans MATTER ,  Martin BOSSART ,  Cecile COMBEAU ,  Christine DELAISI ,  Ingrid SASSOON ,  Anke STEINMETZ ,  Didier BENARD

Inventor： Swen HOELDER ,  Gunter MULLER ,  Karl SCHOENAFINGER ,  David William WILL ,  Hans MATTER ,  Martin BOSSART ,  Cecile COMBEAU ,  Christine DELAISI ,  Ingrid SASSOON ,  Anke STEINMETZ ,  Didier BENARD

IPC: A61K9/28 ,  C07D401/14 ,  A61K31/501 ,  A61K9/12 ,  A61P35/00 ,  A61K31/5377 ,  C07D413/14

CPC classification number: C07D403/04 ,  C07D401/14

Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).

Abstract translation: 公开了根据通式（I）的化合物，其中取代基X，R 1和R 2的定义在说明书中详细描述，以及它们的生理上可接受的盐和溶剂合物，这些化合物的制备方法及其作为药物的用途。 这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂。

公开(公告)号：US20090042880A1

公开(公告)日：2009-02-12

申请号：US12251572

申请日：2008-10-15

Applicant: Swen HOELDER ,  Karl SCHOENAFINGER ,  David William WILL ,  Hans MATTER ,  Gunter MULLER ,  Cecile COMBEAU ,  Christine DELAISI ,  Anke STEINMETZ ,  Ingrid SASSOON

Inventor： Swen HOELDER ,  Karl SCHOENAFINGER ,  David William WILL ,  Hans MATTER ,  Gunter MULLER ,  Cecile COMBEAU ,  Christine DELAISI ,  Anke STEINMETZ ,  Ingrid SASSOON

IPC: A61K31/5377 ,  A61K31/501 ,  C07D401/14 ,  C07D403/14 ,  A61P35/00 ,  C07D471/04 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04

Abstract: Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).

Abstract translation: 公开了通式（I）的化合物，其中取代基A，B，D，E，R 1和R 2的定义在说明书中详细描述，以及其生理上可耐受的盐，这些化合物的制备方法和 它们用作药物。 这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂。

公开(公告)号：US07365088B2

公开(公告)日：2008-04-29

申请号：US10849088

申请日：2004-05-19

Applicant: Marc Nazare ,  Volkmar Wehner ,  Volker Laux ,  Matthias Urmann ,  Armin Bauer ,  Hans Matter

Inventor： Marc Nazare ,  Volkmar Wehner ,  Volker Laux ,  Matthias Urmann ,  Armin Bauer ,  Hans Matter

IPC: A16K31/42 ,  A16K31/4152 ,  C07D261/20 ,  C07D413/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention relates to a compound of the formula I wherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract translation: 本发明涉及式I化合物，其中J 1，J 2，R 0，R 1，O 2， >，R 2，Q，V，G和M如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

公开(公告)号：US20080039489A1

公开(公告)日：2008-02-14

申请号：US11777324

申请日：2007-07-13

Applicant: Manfred SCHUDOK ,  Hans MATTER ,  Armin HOFMEISTER

Inventor： Manfred SCHUDOK ,  Hans MATTER ,  Armin HOFMEISTER

IPC: C07D471/04 ,  A61K31/4355 ,  A61P19/00 ,  A61P35/00 ,  A61P9/00

CPC classification number: C07D491/04

Abstract: The present invention includes novel derivatives of bicyclic tetrahydrofuran imino acids of formula I, processes for their preparation, and uses thereof as medicaments. The compounds are suitable for use in the therapy and prophylaxis of diseases which are associated with an increased matrix metalloproteinase activity.

Abstract translation: 本发明包括式I的双环四氢呋喃亚氨基酸的新衍生物，其制备方法及其作为药物的用途。 该化合物适合用于治疗和预防与增加的基质金属蛋白酶活性有关的疾病。

公开(公告)号：US07317027B2

公开(公告)日：2008-01-08

申请号：US10849089

申请日：2004-05-19

Applicant: Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

Inventor： Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

IPC: A61K31/44 ,  C07D401/00

CPC classification number: C07D471/04

Abstract: The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract translation: 本发明涉及式I化合物，其中R 0，R 1，R 2，R 3，R 3， ，Q，V，G和M如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。